期刊文献+

阿尔茨海默病正电子显像剂^(11)C-6-OH-BTA-1的制备 被引量:8

preparation of amyloid-beta imaging agent ^(11)C-6-OH-BTA-1
下载PDF
导出
摘要 目的研究脑内β-淀粉样蛋白的 PET 显像剂[N-甲基-^(11)C]2-[4′-(甲氨基)苯基]-6-羟基苯并噻唑(^(11)C-6-OH-BTA-1)的制备路线。方法使用^(11)C-三氟甲基磺酰甲烷(Triflate-CH_3)进行^(11)C 标记,分别采用"反应瓶"法和"loop 环"法制备^(11)C-6-OH-BTA-1,应用 C18 cartridge 柱提纯产品。结果 2种方法从加速器开始生产^(11)CO_x 到生成 ^(11)C-6-OH-BTA-1的时间相近,分别为33和32min,按照加速器生产925 MBq^(11)C-Triflate-CH_3计算,未校正^(11)C 衰变的情况下,无色澄清^(11)C-6-OH-BTA-1注射液的产率为16%~44%,放化纯为92%~93%。结论使用"loop 环"法制备^(11)C-6-OH-BTA-1,方法简单易操作。 Objective It is hypothesized that the surplus of amyloid-beta (Aβ) in the brain leads to neuronal degeneration and dementia. A novel PET tracer N-methyl-11^C-2-( 4'-methylaminophenyl ) -6- hydroxybenzothiazole (11^C-6-OH-BTA-1 ) has been reported useful in the evaluation of these Aβ plaques. This study aimed at designing a better preparation method for this PET tracer. Methods 11^C-Triflate-CH3 was bubbled into the reactor of an automated remotely controlled radiosyntbesizer module, which contained reaction materials either in a V-tube or in a loop. The reaction was completed under different conditions. The radiolabelled products were purified by a small solid-phase cartridge. Results The whole preparation process took about 33 min from 11^COx to 11^C-6-OH-BTA-1 by using either method. The radiochemical purity was Between 92% - 93% and radioactivity concentration was over 185 MBq/ml. The loop method achieved a higher productivity than the other method. Conclusion The preparation and purification procedures of 11^C-6-OH-BTA-1 can be more effectively carried out by the captive loop method.
出处 《中华核医学杂志》 CAS CSCD 北大核心 2007年第6期327-329,共3页 Chinese Journal of Nuclear Medicine
基金 2005年上海市引进技术的吸收与创新计划项目(05JYYY-49)
关键词 阿尔茨海默病 碳放射性同位素 同位素标记 6-OH-BTA-1 Alzheimer's disease Carbon radioisotopes Isotope labeling 6-OH-BTA-1
  • 相关文献

参考文献8

  • 1周玲,管一晖,丁正同,蒋雨平.阿尔茨海默病早期β-淀粉样斑块的PET显像诊断[J].中国临床神经科学,2007,15(1):108-112. 被引量:6
  • 2Mathis CA, Holt DP,Wang YM, et al. Lipophilic ^11C-labelled thioflavin-T analogues for imaging amyloid plaques in Alzheimer's disease. J Labelled Comp Radiopharm, 2001,44 Suppl: 26-28.
  • 3张锦明,田嘉禾,王武尚,刘伯里.在线制备^(11)C-Triflate-CH_3[J].同位素,2006,19(2):124-128. 被引量:21
  • 4Solbach C, Uebele M, Reischl G, et al. Efficient radiosynthesis of carbon-ll labelled uncharged thioflavin-T derivatives using [^11C] methyl triflate for β-amyloid imaging in Alzheimer's disease with PET. Appl Radiat Isot, 2005, 62: 591-595.
  • 5Wilson AA,Garcia A,Chestakova A,et al. A rapid one-step radiosynthesis of the β-amyloid imaging radiotracer N-methyl-^11 C-2-4'-methylaminophenyl-6-hydroxybenzothiazole ( ^11C-6-OH-BTA-1 ). J Labelled Comp Radiopharm, 2004, 47: 679-682.
  • 6Mathis CA, Wang YM, Holt DP, et al. Synthesis and evaluation of ^11C-labeled 6-substituted 2-arylbenzothiazoles as amyloid imaging agents. J Med Chem, 2003, 46: 2740-2754.
  • 7Klunk WE, Engler H, Nordberg A, et al. Imaging brain amyloid in Alzheimer's disease with Pittsburgh Compound-B. Ann Neurol, 2004, 55:306-319.
  • 8Mintun MA, LaRossa GN, Sheline YI, et al. ^11C-PIB in a nondemented population potential antecedent marker of Alzheimer disease. Neurology, 2006, 67:446-452.

二级参考文献28

  • 1张锦明,田嘉禾,王武尚,刘伯里.单管法自动化合成^(11)C-碘代甲烷[J].中华核医学杂志,2004,24(4):243-244. 被引量:24
  • 2BOLTON R.Isotopic Methylation[J].J Label Compd Radiopharm,2001,44:701-736.
  • 3MULHOLLAND GK,JEWETT DM,TOORO-NGIAN SA.Routine Synthesis of N-[^11C-methyl]scopolamine by Phosphite Mediated Reductive Methylation With ^11C-formaldehyde[J].Appl Radiat Isot,1988,39:373-376.
  • 4NAGREN K,HALDIN C.Methylation of Amide and Thiol Functions With ^11C-methyl Triflate,as Exemplified by ^11C-NMSP,^11C-Flumazenil and ^11C-methionine[J].Label Compd Radiopharm,1998,41:831-841.
  • 5JEWETT DM.A Simple Synthesis of ^11C-methyl Triflate[J].Appl Radiat Isot,1992,43:1 383-1 385.
  • 6LUNDKVIST C,HALLDIN C,SWAHN CG,et al.Improved Syntheses of the PET Radioligands,^11C-FLB457,^11C-MDL100907 and ^11C-β-CIT-FE by the Used of ^11C-methyl Triflate[J].J Label Compd Radiopharm,1998,41:545-556.
  • 7LANGER O,NAGREN K,DOLLE F,et al.Precursor Synthesis and Radiolabelling of the Dopamine D2 Receptors Ligand ^11C-raclopride From ^11C-methyl Triflate[J].J Label Compd Radiopharm,1999,42:1 183-1 193.
  • 8MOCK BH,MULHOLLAND GK,VAVREK MT.Convenient Gas Phase Bromination of ^11C-methane and Production of ^11C-methyl Triflate[J].Nucl Med Biol,1999,26:467-471.
  • 9Mathis CA,Wang Y,Klunk WE.Imaging β-amyloid plaques and neurofibrillary tangles in the aging human brain[J].Curr Pharm Des,2004,10:1469-1492
  • 10Klunk WE,Wang Y,Huang GF,et al.Uncharged thioflavin-T derivatives bind to amyloid-beta protein with high affinity and readily enter the brain[J],Life Sci,2001,69:1471-1484

共引文献23

同被引文献69

  • 1张锦明,田嘉禾,王武尚,刘伯里.单管法自动化合成^(11)C-碘代甲烷[J].中华核医学杂志,2004,24(4):243-244. 被引量:24
  • 2何跃.老年性痴呆患病率及神经生化标志物的研究现状[J].中国临床康复,2005,9(4):143-145. 被引量:8
  • 3张锦明,田嘉禾,王武尚,刘伯里.在线制备^(11)C-Triflate-CH_3[J].同位素,2006,19(2):124-128. 被引量:21
  • 4周玲,管一晖,丁正同,蒋雨平.阿尔茨海默病早期β-淀粉样斑块的PET显像诊断[J].中国临床神经科学,2007,15(1):108-112. 被引量:6
  • 5Mathis CA, Holt DP, Wang YM, et al. Lipophilic ^11C-labelled thioflavin-T analogues for imaging amyloid plaques in Alzheimer's disease. J Labelled Comp Radiopharm, 2001,44 Suppl: 26-28.
  • 6Masters CL, Cappai R, Barnham KJ, et al. Molecular mechanisms for Alzheimer's disease: implications for neuroimaging and therapeutics. J Neurochem, 2006, 97:1700-1725.
  • 7Klunk WE, Engler H, Nordberg A, et al. Imaging brain amyloid in Alzheimer's disease with Pittsburgh Compound-B. Ann Neurol, 2004, 55: 306-319.
  • 8Petrella JR,Coleman RE. Doraiswamy PM. Neuroimaging and early diagnosis of Alzheimer disease: a look to the future. Radiology, 2003, 226:315-336.
  • 9Salmon E, Sadzot B, Maquet P, et al. Differential diagnosis of Alzheimer's disease with PET. J Nucl Med, 1994, 35:391-398.
  • 10Nussbaum RL, Ellis CE. Alzheimer's disease and Parkinson's disease. N Engl J Med, 2003, 348: 1356-1364.

引证文献8

二级引证文献24

相关作者

内容加载中请稍等...

相关机构

内容加载中请稍等...

相关主题

内容加载中请稍等...

浏览历史

内容加载中请稍等...
;
使用帮助 返回顶部